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Unit 1: Pharm > Alkylating Agents > Flashcards

Alkylating Agents Flashcards

1
Q

What is the mechanism of action in alkylating agents?

A
  • produce strong electrophiles through carbonium or ethyleneimonium ion intermediates
  • these covalently bind via alkylation of nucleophilic moieties in DNA
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2
Q

What is the most common site of alkylation?

A

N7 Position of guanine

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3
Q

Are alkylating agents cell cycle specific or nonspecific?

A

nonspecific

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4
Q

What are some side effects of alkylating agents?

A
  • BM supression
  • mucosal toxicity
  • nausea and vomiting
  • toxic effects on repro systems
  • inc leukemic risk
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5
Q

How does resistance develop to alkylating agents?

A
  • decreased permeability or uptake
  • inc rates of catabolism
  • inc DNA repair
  • inc glutathione production
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6
Q

How does glutathione act on alkylating agents?

A

inactivates via conjugation

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7
Q

Name 3 types of nitrogen mustards?

A
  1. mechlorethamine - mustargen
  2. cyclophosphamide - cyclotoxan
  3. ifofasmide -Ifex
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8
Q

Where is mechlorethamine converted to an active metabolite?

A

body fluids or enzymatically converted in the liver

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9
Q

What is mechlorethamine used for?

A
  • Hodkins disease

- topically for treatment of cutaneous T cell lymphoma

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10
Q

Why isnt mechlorethamine used much anymore?

A

it causes sterility

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11
Q

Where is cyclophosphamide and ifosfamide converted to an active metabolite?

A

in the liver by: hepatic cyt P450

-converted to phosphoramide mustard

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12
Q

What is cyclophosphamide used to treat?

A
  • ALL
  • CLL
  • non hodkins lymphoma
  • breast cancer
  • lung cancer
  • ovarian cancer
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13
Q

How are hemorrhagic cysts in the bladder prevented when a patient receives cyclophosphamide or ifosfamide?

A

adequate hydration and treatment with MESNA

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14
Q

By what method is cyclophosphamide and ifosfamide administered?

A

orally - relatively long half life 7-15 hours

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15
Q

What is ifosfamide used to treat?

A
  • sarcoma

- testicular cancer

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16
Q

Which drugs have the side effect of hemorrhagic cysts in the bladder? Why does this occur?

A

cyclophosphamide and ifosfamide

17
Q

What are two drugs of the nitrosureas category of alkylating agents?

A
  • carmustine and Lomustine
18
Q

What are carmustine and lomustine used to treat?

A

brain tumors - crosses the BBB

19
Q

What are some serious side effects of nitrosureas ?

A
  • renal toxicity
  • pulmonary fibrosis
  • profound myelosuppression
  • severe nausea and vomiting
20
Q

What are the three drugs that belong to the category of alkylating agents: triazenes?

A
  1. dacarbazine
  2. procarbazine
  3. temozolamide
21
Q

Where is dacarbazine activated?

A

prodrug activated by liver cytochromes

22
Q

What is the method of action of procarbazine?

A

forms free fradicals

23
Q

What is the method of activation of temozolomide?

A

nonenzymatic conversion to methylhydrazine at physio pH

24
Q

What is dacarbazine used to treat?

A

part of ABVD for hodkins disease

-also used for malignant melanoma

25
Q

What is procarbazine used to treat?

A

hodkins lymphoma

26
Q

What is temozolomide used to treat?

A

malignant gliomas

27
Q

What are some side effects of dacarbazine and temozolomide?

A
  • nausea and vomiting
  • myelosupression
  • flu like symptoms
28
Q

How is dacarbazine administered?

A

by IV

29
Q

How is temozolomide administered?

A

taken orally

30
Q

What is a serious side effect of procarbazine?

A

may cause leukemia

31
Q

What are the three drugs that belong to the platinum analog category of alkylating agents?

A
  1. cisplatin
  2. carboplatin
  3. oxaliplatin
32
Q

How do platinum analogs work?

A

alkylating agents that do NOT form carbonium intermediates or alkylate DNA

  • covalently bind nucleophilic sites on DNA
  • converted to active cytotoxic forms by reacting with water and becoming + charged hydrated intermediates

-form inter and intrastrand cross links

33
Q

What is cisplatin used to treat?

A
  • testicular
  • ovarian and cervical
  • bladder
  • Head and neck
  • lung carcinoma
34
Q

What are some toxicities of cisplatin?

A
  • nephrotoxicity
  • ototoxicity
  • peripheral neuropathies at high doses

-severe nausea and vomiting

35
Q

What is carboplatin used to treat?

A

ovarian cancer

36
Q

What is a side effect of carboplatin?

A

myelosupression

37
Q

What is oxaliplatin used to treat?

A

gastric and colorectal cancer

38
Q

What are side effects of oxaliplatin?

A

peripheral sensory neuropathy - cold induced

-neutropenia

Unit 1: Pharm (8 decks)

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